EP0689427B1 - Wasserdispersible therapeutische carotenoid verbindungen - Google Patents

Wasserdispersible therapeutische carotenoid verbindungen Download PDF

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Publication number
EP0689427B1
EP0689427B1 EP94911015A EP94911015A EP0689427B1 EP 0689427 B1 EP0689427 B1 EP 0689427B1 EP 94911015 A EP94911015 A EP 94911015A EP 94911015 A EP94911015 A EP 94911015A EP 0689427 B1 EP0689427 B1 EP 0689427B1
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EP
European Patent Office
Prior art keywords
carotene
composition according
beta
therapeutic composition
weight
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
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EP94911015A
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English (en)
French (fr)
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EP0689427A1 (de
EP0689427A4 (de
Inventor
Lance Elliott Schlipalius
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Cognis Australia Pty Ltd
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Cognis Australia Pty Ltd
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Publication of EP0689427A1 publication Critical patent/EP0689427A1/de
Publication of EP0689427A4 publication Critical patent/EP0689427A4/de
Application granted granted Critical
Publication of EP0689427B1 publication Critical patent/EP0689427B1/de
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A61K9/1274—Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases, cochleates; Sponge phases
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Claims (22)

  1. Therapeutische Zusammensetzung, dadurch gekennzeichnet, dass die Zusammensetzung als Injektionspharmakon zubereitet ist und folgendes umfasst:
    (a) wenigstens 30 Gew.-% einer wasserlöslichen oder -dispergierbaren Komponente;
    (b) eine Emulgatorkomponente, die aus Mono- und Diglyceridstrukturen pflanzlicher und tierischer Herkunft, Lecithinen und Phospholipiden ausgewählt ist;
    (c) ein wasserunlösliches therapeutisches Mittel in einem geeigneten Trägermedium, wobei das wasserunlösliche therapeutische Mittel eine Carotinoidzusammensetzung umfasst, die beta-Carotin enthält, und das als Träger für das wasserunlösliche therapeutische Mittel verwendete Trägermedium aus der Gruppe ausgewählt ist, die aus Fettsäuren und Triglyceridlipiden und nichtverseifbaren Lipidpräparaten, Erdölkohlenwasserstoffen einschließlich Octadecan und Kombinationen der obigen Verbindungen besteht.
  2. Therapeutische Zusammensetzung gemäß Anspruch 1, wobei die wasserlösliche oder -dispergierbare Komponente aus Zuckeralkoholen, Zuckern, Aminosäuren, Wasser, Vitaminen, Blutserum oder -plasma, Lymphe, Puffern und Kombinationen und Polymeren dieser Materialien, und Injektionsgrundlagen, wie Mineralsalzpräparaten und Dextroselösungen, oder Kombinationen dieser Komponenten ausgewählt ist.
  3. Therapeutische Zusammensetzung gemäß Anspruch 1 oder 2, wobei die wasserlösliche oder -dispergierbare Komponente im Bereich von 30 bis 90 Gew.-% liegt.
  4. Therapeutische Zusammensetzung gemäß Anspruch 1, 2 oder 3, wobei es sich bei der wasserlöslichen oder -dispergierbaren Komponente um Glycerin handelt.
  5. Therapeutische Zusammensetzung gemäß Anspruch 4, wobei das Glycerin im Bereich von 30 bis 90 Gew.-% liegt.
  6. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 5, wobei das Glycerid der Emulgatorkomponente Glycerylmonooleat ist.
  7. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 6, wobei der Emulgator im Bereich von 0,2 bis 20 Gew.-% liegt.
  8. Therapeutische Zusammensetzung gemäß Anspruch 7, wobei der Emulgator im Bereich von 1,0 bis 10 Gew.-% liegt.
  9. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 8, wobei die Carotinoidzusammensetzung wenigstens 85 Gew.-% beta-Carotin enthält.
  10. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 8, wobei die Carotinoidzusammensetzung 85 bis 90 Gew.-% beta-Carotin enthält.
  11. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 10, wobei die Carotinoidzusammensetzung 10 bis 15 Gew.-% Oxycarotinoide und alpha-Carotin enthält.
  12. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 11, wobei das beta-Carotin cis-beta-Carotin und all-trans-beta-Carotin umfasst.
  13. Therapeutische Zusammensetzung gemäß Anspruch 12, wobei der Gehalt des beta-Carotins an cis-beta-Carotin im Bereich von 50 bis 90% liegt.
  14. Therapeutische Zusammensetzung gemäß Anspruch 13, wobei der Gehalt des beta-Carotins an cis-beta-Carotin im Bereich von 70 bis 85% liegt.
  15. Therapeutische Zusammensetzung gemäß einem der Ansprüche 12 bis 14, wobei es sich bei dem cis-beta-Carotin vorwiegend um 9-cis-beta-Carotin handelt.
  16. Therapeutische Zusammensetzung gemäß einem der Ansprüche 12 bis 15, wobei das cis-beta-Carotin zu 60 bis 90% aus 9-cis-beta-Carotin besteht.
  17. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 16, wobei das wasserunlösliche therapeutische Mittel im Bereich von 0,1 bis 10 Gew.-% der Zubereitung liegt.
  18. Therapeutische Zusammensetzung gemäß Anspruch 17, wobei das wasserunlösliche therapeutische Mittel im Bereich von 1 bis 5 Gew.-% der Zubereitung liegt.
  19. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 18, wobei die Triglyceridlipide aus der Gruppe ausgewählt sind, die aus Fetten und/oder Ölen besteht, die aus pflanzlichen Quellen stammen, einschließlich Samenölen, wie Sojaöl, Baumwollsaatöl und Sonnenblumenöl, und aus tierischen Quellen stammen, einschließlich Fisch und Rind.
  20. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 19, wobei das Trägermedium im Bereich von 0,1 bis 40 Gew.-% liegt.
  21. Therapeutische Zusammensetzung gemäß Anspruch 20, wobei das Trägermedium im Bereich von 1 bis 20 Gew.-% liegt.
  22. Therapeutische Zusammensetzung gemäß einem der Ansprüche 1 bis 21, wobei die Zubereitung weiterhin mit Verdünnungsmitteln verdünnt ist, die aus der Gruppe ausgewählt sind, die aus wässrigen Puffern, normalen intravenösen Präparaten (einschließlich isotonischer Kochsalzlösung oder 5%iger Dextroselösung) und Blutserum sowie Kombinationen davon besteht.
EP94911015A 1993-03-22 1994-03-22 Wasserdispersible therapeutische carotenoid verbindungen Expired - Lifetime EP0689427B1 (de)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
AUPL7935/93 1993-03-22
AUPL793593 1993-03-22
AUPL793593 1993-03-22
PCT/AU1994/000143 WO1994021232A1 (en) 1993-03-22 1994-03-22 Water dispersible therapeutic compounds

Publications (3)

Publication Number Publication Date
EP0689427A1 EP0689427A1 (de) 1996-01-03
EP0689427A4 EP0689427A4 (de) 1998-04-15
EP0689427B1 true EP0689427B1 (de) 2002-06-12

Family

ID=3776794

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94911015A Expired - Lifetime EP0689427B1 (de) 1993-03-22 1994-03-22 Wasserdispersible therapeutische carotenoid verbindungen

Country Status (8)

Country Link
US (1) US5773026A (de)
EP (1) EP0689427B1 (de)
JP (1) JPH08510995A (de)
AT (1) ATE218855T1 (de)
AU (1) AU696956B2 (de)
DE (1) DE69430799T2 (de)
ES (1) ES2178651T3 (de)
WO (1) WO1994021232A1 (de)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU660630B2 (en) * 1990-10-01 1995-07-06 Brigham And Women's Hospital Beta-carotene and vitamin E therapy for inhibition of major vascular events
US6132790A (en) * 1991-09-06 2000-10-17 Betatene Limited Carotenoid composition
AU700249B2 (en) * 1994-04-08 1998-12-24 Cognis Australia Pty Ltd Carotenoid agent for inhibiting the conversion of epithelial cells to tumours
AUPM493194A0 (en) * 1994-04-08 1994-05-05 Buckmeier, Julie A. Therapeutic agent for inhibiting the conversion of epithelial cells to tumours
ES2180636T3 (es) * 1994-05-20 2003-02-16 Novavax Inc Emulsiones antimicrobianas de aceite en agua.
DE19609476A1 (de) * 1996-03-11 1997-09-18 Basf Ag Stabile zur parenteralen Verabreichung geeignete Carotinoid-Emulsionen
AU5719798A (en) * 1996-12-31 1998-07-31 Inhale Therapeutic Systems, Inc. Processes for spray drying aqueous suspensions of hydrophobic drugs with hydrophilic excipients and compositions prepared by such processes
EP0984915A4 (de) 1997-04-04 2002-11-27 Henkel Corp Luteinester mit hoher bioverfügbarkeit
US6767342B1 (en) 2001-04-23 2004-07-27 Evelyna D. Cantwell Oxygen bandage system
US7375133B2 (en) * 2002-07-29 2008-05-20 Cardax Pharmaceuticals, Inc. Pharmaceutical compositions including carotenoid ether analogs or derivatives for the inhibition and amelioration of disease
US20050009788A1 (en) * 2002-07-29 2005-01-13 Lockwood Samuel Fournier Carotenoid ester analogs or derivatives for controlling connexin 43 expression
CA2495167C (en) * 2002-07-29 2018-08-21 Hawaii Biotech, Inc. Structural carotenoid analogs for the inhibition and amelioration of disease
US7345091B2 (en) * 2002-07-29 2008-03-18 Cardax Pharmaceuticals, Inc. Carotenoid ether analogs or derivatives for the inhibition and amelioration of disease
US7320997B2 (en) * 2002-07-29 2008-01-22 Cardax Pharmaceuticals, Inc. Pharmaceutical compositions including carotenoid ester analogs or derivatives for the inhibition and amelioration of disease
US7723327B2 (en) * 2002-07-29 2010-05-25 Cardax Pharmaceuticals, Inc. Carotenoid ester analogs or derivatives for the inhibition and amelioration of liver disease
US7763649B2 (en) * 2002-07-29 2010-07-27 Cardax Pharmaceuticals, Inc. Carotenoid analogs or derivatives for controlling connexin 43 expression
US20050148517A1 (en) * 2002-07-29 2005-07-07 Lockwood Samuel F. Carotenoid ether analogs or derivatives for controlling connexin 43 expression
US8088363B2 (en) 2002-10-28 2012-01-03 Zeavision Llc Protection against sunburn and skin problems with orally-ingested high-dosage zeaxanthin
WO2005102356A1 (en) * 2004-04-14 2005-11-03 Hawaii Biotech, Inc. Carotenoid analogs or derivatives for the inhibition and amelioration of inflammation
US20060058269A1 (en) * 2004-04-14 2006-03-16 Lockwood Samuel F Carotenoid analogs or derivatives for the inhibition and amelioration of inflammation
US7351424B2 (en) * 2004-07-22 2008-04-01 Bio Lut S.A. De C.V. Enhanced purity trans-lutein-ester compositions and methods of making same
US20070065487A1 (en) * 2005-09-21 2007-03-22 Bio Lut S.A. De C.V. Trans-lutein xantophyll ester of high purity and high bioavailability in micellar solution and a process for the preparation thereof
GB0523431D0 (en) * 2005-11-17 2005-12-28 Inst For Akvakulturforskning A Method
WO2010127408A1 (en) * 2009-05-07 2010-11-11 Huntsman Corporation Australia Pty. Limited Dispersants in high-electrolyte solutions

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AU595824B2 (en) * 1985-08-30 1990-04-12 Betatene Limited Narurally-derived carotene/oil composition and the process for the production thereof by direct extraction of carotene from algae
US4680314A (en) * 1985-08-30 1987-07-14 Microbio Resources, Inc. Process for producing a naturally-derived carotene/oil composition by direct extraction from algae
WO1989006977A1 (en) * 1988-02-04 1989-08-10 Board Of Regents, The University Of Texas System Formulation and use of retinoids in treatment of cancer and other diseases
JPH0225418A (ja) * 1988-07-14 1990-01-26 Kyorin Pharmaceut Co Ltd イブジラスト脂肪乳剤およびその製造方法
DE3903056A1 (de) * 1989-02-02 1990-08-09 Braun Melsungen Ag Fettemulsion zur intraperitonealen applikation, ihre herstellung und anwendung
GB8919172D0 (en) * 1989-08-23 1989-10-04 Univ Nottingham Useful composition
AU660630B2 (en) * 1990-10-01 1995-07-06 Brigham And Women's Hospital Beta-carotene and vitamin E therapy for inhibition of major vascular events
DE4031094A1 (de) * 1990-10-02 1992-04-09 Basf Ag Verfahren zur herstellung von stabilen injizierbaren (beta)-carotin-solubilisaten
PH31204A (en) * 1990-11-02 1998-05-05 Fujisawa Pharmaceutical Co Pharmaceutical composition.
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EP0602137B1 (de) * 1991-09-06 2002-01-23 Cognis Australia Pty Ltd Carotinoide zusammensetzung
EP0621773B1 (de) * 1992-01-16 1998-11-25 The Board Of Regents, The University Of Texas System Formulierung und verwendung von carotenoiden in der krebsbehandlung
DE69327100T2 (de) * 1992-06-04 2000-04-13 Betatene Pty Ltd Gemisch mit hohem gehalt an cis beta-carotin

Also Published As

Publication number Publication date
WO1994021232A1 (en) 1994-09-29
ES2178651T3 (es) 2003-01-01
EP0689427A1 (de) 1996-01-03
DE69430799D1 (de) 2002-07-18
DE69430799T2 (de) 2003-02-13
US5773026A (en) 1998-06-30
JPH08510995A (ja) 1996-11-19
ATE218855T1 (de) 2002-06-15
EP0689427A4 (de) 1998-04-15
AU696956B2 (en) 1998-09-24
AU6370594A (en) 1994-10-11

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